Discovery of drug-like inhibitors of an essential RNA-editing ligase in Trypanosoma brucei.

@article{Amaro2008DiscoveryOD,
  title={Discovery of drug-like inhibitors of an essential RNA-editing ligase in Trypanosoma brucei.},
  author={Rommie E. Amaro and Achim Schnaufer and Heidrun Interthal and W. C. Hol and Kenneth D. Stuart and James Andrew McCammon},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={2008},
  volume={105 45},
  pages={17278-83}
}
Trypanosomatid RNA editing is a unique process and essential for these organisms. It therefore represents a drug target for a group of protozoa that includes the causative agents for African sleeping sickness and other devastating tropical and subtropical diseases. Here, we present drug-like inhibitors of a key enzyme in the editing machinery, RNA-editing ligase 1 (REL1). These inhibitors were identified through a strategy employing molecular dynamics to account for protein flexibility. A… CONTINUE READING